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Aniracetam

Aniracetam is an Amapakine nootropic of the racetam family. Aniracetam is also referred to as 1-p-Anisoyl-2-pyrrolidinone, 1(4-Methoxybenzoyl)-2-pyrrolidinone, Ro 13-5057, CAS 72432-10-1, Sarpul, Draganon, Ampamet, Referan, Memodrin. As a racetam and AMPAkine nootropic, it is closely related to Piracetam, but Aniracetam is to some extent more potent than Piracetam. The substance is synthesized by reacting Anisoyl chloride with 2-Pyrrolidone or GABA. In addition to being fat (lipid) soluble, Aniracetam is Cholinergic and has a half-life that is significantly shorter compared to other racetams. Aniracetam was widely employed as a parent compound in the development of the new nootropic class of Ampakine drug.

Aniracetam was originally developed by a Belgian Chemist, Hoffmann La-Roche, in the 1970's. The discovery of piracetam was the pioneering development of the racetams nootropics and Aniracetam is a derivative of Piracetam. As a result, the chemical structure in the two racetams is similar compared to the other nootropic agents that have a 5 carbon oxo-pyrrolidine ring. Aniracetam is a pyrrolidinone compound that contains an anisoyl ring with an O-methoxy group located at its lone para position that replaces the amino group found in the Piracetam structure. In other words, Aniracetam is simply a piracetam molecule that contains a methylated phenyl group as a substitute to the amine group, this alteration was meant to improve fat solubility, and it is responsible for the differences between Aniracetam and Piracetam. The chemical formula for Aniracetam is C12h13NO3. The substance is commonly used as a Nootropic agent.

Details

HISTORY

Aniracetam is an original product of Hoffman La Roche, a subsidiary company of the Roche Holding AG. Despite holding the U.S. patent on Aniracetam, the corporation has tried to get approval from the US Food and Drug Administration (FDA) but has not been able to prove that the substance can act as a drug due to the high criteria set by the FDA. This is irrespective of the fact that Aniracetam has a long list of potential positive effects. Being closely related to Piracetam in terms of chemical structure, the two substances have been compared in studies. These studies found Aniracetam to be more efficient in the treatment of a wider range of conditions compared to Piracetam. Aniracetam is as such more potent/powerful than Piracetam.

The substance (aniracetam) has its effects on the central nervous system whereby it stimulates memory and learning processes. There are numerous scientific studies carried out to test the health effects of Aniracetam in the treatment of various cerebral dysfunctional disorders. However, a majority of these pharmacological studies were animal experiments. These animal studies showed that Aniracetam is safe and efficient in treating emotional problems, cognitive impairment, sleep problems and additional behavioral problems. As a result, some clinical trials have been conducted to discover the effects of Aniracetam on the human brain.

CLINICAL STUDIES

Studies carried out by pharmacologists have indicated that Aniracetam stimulates/ acts on the functions of the central neuronal receptors by using glutamic acid to cause memorization processes in the AMPA receptors and protection of the metabotropic receptors (nerve cells). Several clinical studies have also shown particular therapeutic activities influenced by the manipulation of the cognitive functions. These studies have shown improvements in memory (both short term and long term), learning, reasoning, attention span, concentration, alertness, and absent-mindedness. In lab animals, Aniracetam has shown to particularly lower the rate of receptor desensitization in the hippocampus. This implies possible assistance in memory formation, and it does not interfere with choline take-up into hippocampal cells and additionally promotes acetylcholine release.

Human studies have revealed that Aniracetam is a very powerful cognitive enhancer. The human subjects involved in one particular study had improvements in their scores after taking a number of memory and intelligence tests after they had undergone Aniracetam therapy (Saletu, 1980, 1984). Aniracetam has the potential to enhance what the brain has memorized and assists the mind to achieve a state of concentration. It functions by stimulating the Acetylcholine receptors and increasing the focus and energy in the human brain. As a result, the mind has the capabilities to increase the rate of processing and progressing memory. Apart from improving cognition, Aniracetam has positive effects on several other variables. In post-stroke depression and sleeping disorder therapy and Alzheimer's, Cerebral infarction and Parkinson's, it lowers anxiety and depression. To ascertain the ability of Aniracetam to cause improvements in Alzheimer's patients when administered as treatment, a study was carried out in which Aniracetam efficiency was compared to that of acetylcholine stares inhibitors. The study showed that there was no sufficient evidence to prove the efficiency differences among the cognitive improvements. However, the study proved that Nootropic agents have the ability to enhance cognition in individuals with Alzheimer's condition.

Another study was conducted by a group of researchers who were seeking to study the effects of Aniracetam in treating insomnia. They combined Aniracetam with Zopiclone and administered the combination drug therapy to 9 insomnia patients (Individuals had been diagnosed with insomnia linked to cerebrovascular and non-cerebrovascular problems). An analysis of the results from the study showed that 78% of the individuals who participated in the study reported that the combination therapy was effective in prolonging sleep.

Studies carried out to test the effect of Aniracetam on Dementia showed positive results. Dementia is a common cognitive disorder that has severe implications. Pharmacologists tested the efficiency of Aniracetam, which has glutamatergic mechanisms and neuroprotective potential when administered for dementia. When it was administered to mental disorder patients, the results showed that it had potential as a treatment option that can be used in people with mild cognitive deficits. Additionally, the results indicated that it is capable of preserving all recognized neuropsychological parameters and at the same time enhance emotional stability in demented patients.

Studies were also conducted to ascertain whether Aniracetam has anti-visual hallucination effects. Researchers picked a study population that comprised of elderly persons aged between 70 to 80 years who had been diagnosed with Parkinson's disease and diffused Levy body disease and administered Aniracetam to them. When the results of the treatment were evaluated, they indicated noticeable improvements in the visual hallucination in these patients. Moreover, the patients did not any adverse effects observed after undergoing the Aniracetam treatment. The study concluded that Aniracetam is an efficient treatment for anti-visual hallucination that does not cause any adverse reactions despite being administered in high dosage therapies. Progressive Supranuclear Palsy (PSP) is yet another condition for which Aniracetam effects were studied. PSP is a rare degenerative disorder that exhibits symptoms not restricted to nuchal dystopia, dementia, vertical gaze palsy and Parkinsonism. The disease is traditionally treated using doses of noradrenaline precursor, levodopa, droid opts, anti-cholinergic, and tricyclic antidepressants drugs. Since Aniracetam has anti-cholinergic properties, two individuals diagnosed with PSP were administered with the substance. This study demonstrated that Aniracetam was capable of enhancing motor function, intellectual function, body balance and volition.

Several studies have shown that Aniracetam provides protection against excitotoxicity, and also provides other neuroprotective effects that include reducing the formation of free radicals and enhancing the metabolism of glucose. In cases that involve neuronal injury, the substance may help in the release of inhibitory neurotransmitters. Animal experiments indicated that the substance has a protective effect on the brain. Additionally, a study carried out in a nursing home involving 60 gastric patients showed that Aniracetam had considerable "revitalizing" result (Forltyn, 1982).

In another animal study, Aniracetam effects on Fetal Alcohol Syndrome (FAS) were studied. Rats were used as study subjects, and Aniracetam was used to improve various cognitive deficits during the onset of FAS in the hippocampus. Irrespective of these studies, Aniracetam's pharmacodynamics, is not well established. Although it may be effective in treating the cerebrovascular disorders and neurological disorders explained above, the use the substance should be subjected to prior approval by a qualified physician. As noted, clinical studies conducted on Aniracetam have not been sufficient, and they require further trials and researches involving larger populations of subjects.